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EP3568130A1 - Compositions pour réduire l'appétit et l'état de manque, augmenter la satiété, améliorer l'humeur et réduire le stress - Google Patents

Compositions pour réduire l'appétit et l'état de manque, augmenter la satiété, améliorer l'humeur et réduire le stress

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Publication number
EP3568130A1
EP3568130A1 EP18700405.6A EP18700405A EP3568130A1 EP 3568130 A1 EP3568130 A1 EP 3568130A1 EP 18700405 A EP18700405 A EP 18700405A EP 3568130 A1 EP3568130 A1 EP 3568130A1
Authority
EP
European Patent Office
Prior art keywords
extract
mangiferin
cyperus esculentus
composition
norathyriol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP18700405.6A
Other languages
German (de)
English (en)
Inventor
Miguel JIMÉNEZ DEL RÍO
Julia C. WIEBE
Laura LÓPEZ RÍOS
Tanausú VEGA MORALES
Rubén PÉREZ MACHÍN
Álvaro SÁNCHEZ RODRÍGUEZ
Carlos J. Mateos
Nigel Peter Gericke
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nektium Pharma SL
Original Assignee
Nektium Pharma SL
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Filing date
Publication date
Application filed by Nektium Pharma SL filed Critical Nektium Pharma SL
Publication of EP3568130A1 publication Critical patent/EP3568130A1/fr
Withdrawn legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/89—Cyperaceae (Sedge family)
    • A61K36/8905—Cyperus (flatsedge)
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/22—Anacardiaceae (Sumac family), e.g. smoketree, sumac or poison oak
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
    • A23V2200/30—Foods, ingredients or supplements having a functional effect on health
    • A23V2200/322—Foods, ingredients or supplements having a functional effect on health having an effect on the health of the nervous system or on mental function
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30—Extraction of the material
    • A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30—Extraction of the material
    • A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Definitions

  • This disclosure relates generally to compositions which reduce craving for unhealthy foods, sweetened beverages and confections, nicotine-containing products, or alcohol without causing undesired physical or psychological side effects, while simultaneously enhancing mood and reducing stress.
  • This disclosure relates to a composition that reduces craving and serves as a substitute for appetite-reducing and smoking-cessation drugs.
  • This new combination contains a plant extract of Tigernut, also known as Chufa (Cyperus esculentus), and an extract containing the xanthonoid compound mangiferin which might be of different origin.
  • the mangiferin-containing extract might be a Mango fruit, bark or leaf extract, Honeybush tea, or an extract of coffee leaves.
  • Tobacco containing the addictive alkaloid nicotine, is highly addictive and one of the most widely abused drugs in the world. According to the WHO worldwide about 1 billion males and 250 million females smoke. Half of them, 5.4 million per year worldwide, eventually die as a direct consequence of their tobacco addiction.
  • the positive reinforcing effects of smoking include mild euphoria, relaxation, and improved attention and working memory, while discontinuation of smoking leads not only to nicotine withdrawal but also to depressed mood, increased stress, irritability, anxiety, and impaired memory and attention, increasing the risk for relapse to smoking.
  • the pharmaceutical drug Rimonabant a cannabinoid receptor CB1 inverse agonist/antagonist, decreases nicotine-taking and nicotine-seeking in rodents.
  • Rimonabant has been shown to improve the ability of smokers to quit smoking in randomized clinical trials, but has been withdrawn from the market due to its severe psychiatric side effects and increased suicidal risk.
  • the side effects of Rimonabant are due to the reduction in the mood-enhancing and de-stressing activities of the endocannabinoid and endogenous opiate systems, and decrease in the elevation of dopamine, induced by nicotine and food in the brain reward area, thereby leading to depression.
  • a potential mood-enhancing pharmaceutical treatment for smoking cessation is Selegiline, a selective and irreversible monoamine oxidase B inhibitor with an ti -depressive activity mainly used as neuroprotector in Parkinson's disease patients. Selegiline primarily affects dopamine levels in the brain, but cholinergic input affects nicotine-induced dopaminergic activity. Scientific evidence from 2013 suggests that targeting craving during early abstinence and adding mood management to behavioral support may improve cessation outcomes in smokers.
  • Smoking cessation is often accompanied by metabolic changes including increased ⁇ -cell secretion in response to glucose and fasting insulin resistance. These alterations may be associated with or contribute to the body weight gain after smoking cessation, which is reportedly a major reason why many smokers relapse after initiating smoking cessation, followed by the accompanying low mood and depression related to the missing reward response.
  • the present combination decreases craving, increases the electroencephalographic signaling of the neurotransmitters dopamine and serotonin, thereby attenuating the reduced reward response, and simultaneously improves mood and decreases emotional stress.
  • calorie restriction is the only physiological intervention known to have a consistent and predictable effect on maintaining health and reducing the risk of disease, improving quality of life and healthspan, and retarding ageing, as demonstrated in multiple studies across diverse animal models.
  • Many hormonal signals from peripheral tissues contribute to the regulation of energy homeostasis and food intake.
  • These regulators including leptin, insulin, and ghrelin, modulate the orexigenic and anorexigenic neuropeptide expression in hypothalamic nuclei.
  • a negative energy balance seems to promote the activity of specific populations of neurons in these hypothalamic nuclei that drive hunger.
  • Methylphenidate the most frequently used medication for the treatment of attention- deficit/hyp eractivity disorder (ADHD).
  • ADHD attention- deficit/hyp eractivity disorder
  • Methylphenidate selectively binds to and inhibits the dopamine transporter, thus increasing brain dopamine levels, which mediate the reward value of food, shortly after oral administration. This effect underscores the importance of central dopamine signaling on eating behavior. Regulation of food intake
  • Regions and networks of the human brain involved in eating behaviour and appetite control have been identified with neuroimaging techniques such as functional MRI, PET, electroencephalography, and magnetoencephalography.
  • Hormones that regulate our drive to eat e.g., leptin, insulin, and glucagon-like peptide-1) can affect brain function.
  • the central nervous system controls appetite and body weight regulation in a rather complicated manner.
  • the human brain integrates internal and external inputs to modulate energy homeostasis.
  • homeostatic control by the hypothalamus is considered to be primarily responsible for controlling appetite, food intake, body weight and the development of obesity.
  • the hypothalamic region is controlled by multiple signals coming from digestive tract, adipose tissue and pancreas in form of leptin, cholecystokinin (CCK), ghrelin, incretins, orexin, insulin, peptide YY, glucose, amino acids and fatty acids, reflecting the physiological situation of the body.
  • CCK cholecystokinin
  • the so-called reward effect a physiological process associated with food intake, is related to the hypothalamus and several other brain regions, including the limbic region and the frontal cortex.
  • the limbic region includes the nucleus accumbens, amygdalae and hippocampus.
  • the neurotransmitter system of the frontal cortex responds to dopamine, serotonin, opioids, and cannabinoids, and is closely related to the reward system and the homeostasis of regulation of food intake. Neurotransmitters
  • VTA ventral tegmental area
  • nucleus accumbens nucleus accumbens
  • dorsal striatum frontal cortex
  • limbic regions e.g., the hippocampus
  • amygdalae amygdalae
  • lateral hypothalamus e.g., the hippocampus
  • Neurotransmitter receptors and transporters represent main targets of drugs in the central nervous system. Interaction of drugs with these molecules induces a signaling cascade, which finally ends up with the control of ion channel conductance. Since the electric activity of single neurons depends on the set of momentarily active ion channels, communication between neurons is governed by channel activity. From here, it is obvious that electrical field potentials reflect the information of larger local networks of electrically active neurons, by representing the interaction of drugs with their targets within the concert of neurotransmission including complex modulation from feedback loops. Frequency analysis of the field potentials in the presence of drugs leads to the so-called electropharmacogram, which has been widely used to characterize drug actions on rat and human brains.
  • Beta waves 13—29.99 Hz
  • beta-1 waves range from 13-20 Hz during daily activity
  • beta-2 and beta-3 waves indicates stress, excessive concentration, and anger.
  • CNS stimulants have been found to influence brain wave activity. It is well known in the art that the attenuation or stimulation pattern and type of brain wave activity reflects underlying brain activities including attention and depression. The anatomical location of the activity can also be related to specific brain functions, for example activation of memory through activation of the hippocampus. Sleepiness and/ or fatigue, for example, have been shown to be correlated to a significant increase of alpha wave activity and a decrease of gamma wave activity. Papadelis et al., Proceedings of the 28th IEEE EMBS Annual International Conference, New York City, USA, Aug 30-Sept 3, 2006, pp. 6201- 6204.
  • Increased gamma-band EEG activity is associated with states of high arousal, alertness, or attention. Attenuation of alpha- and beta-activity in the in-vivo EEG from implanted brain electrodes generally correlate to an increase in neurotransmission, resulting in increased alertness, stimulation and anti-depressant effects.
  • the midbrain dopamine center comprises a key network for reward, salience, motivation, and mood and decreased serotonin metabolism and functioning in the central nervous system is associated with depression.
  • Specific neurotransmitter release can be related to antidepressant and antianxiety effect, as shown for serotonin-dopamine activity modulating drugs like Brexpiprazole or the serotonin and norepinephrine reuptake inhibitor (SNRI) ZBH2012001.
  • serotonin-dopamine activity modulating drugs like Brexpiprazole or the serotonin and norepinephrine reuptake inhibitor (SNRI) ZBH2012001.
  • a composition that suppresses slow wave brain wave activity e.g., theta and/ or alpha- 1 wave brain wave activity, or elevates alpha-2 activity relative to alpha- 1 activity, may act to suppress the effects of nicotine withdrawal, and help a user reduce or stop smoking.
  • compositions useful for: reducing craving and appetite mainly craving and appetite for calories dense sweet or fatty foods, sweet beverages and confections, and craving for smoking
  • prolonging the duration of satiety after eating reducing appetite; reducing weight gain after smoking-cessation, and reducing relapse rate after smoking.
  • these compositions improve mood, and act as anti-depressants, and thereby countering the severe mood side effects of craving and appetite reducing products like Rimonabant.
  • compositions disclosed herein reduce craving and appetite for calorie-dense foods, snacks and beverages, reduce craving for smoking, and do not cause nervousness, anxiety or depression, offers a CNS-activating effect and serve to maintain health and prolong healthspan and lifespan by promoting calorie restriction from reduced craving for calorie-dense foods, snacks, sweet beverages and confections, and reduced craving for cigarettes in smokers, and reduced craving for alcohol.
  • compositions disclosed herein provide reduced appetite and craving, enhanced satiety, decreased stress, and increased mood over a relatively extended period of time, but are substantially free of side effects and have no addictive potential, so they can be consumed over a long period of time by any person or mammal.
  • compositions disclosed herein may be included in food and beverage products including snack bars, chewing gum, confections, meal-replacement shakes, smoothies, beverages, chocolate and energy-drinks used for anti-craving, and enhanced satiety purposes to:
  • Tigernuts have been shown in animal models to improve serum lipid profiles and reduce elevated serum glucose, while mangiferin has been shown to prevent hyperglycemia, and have antihyp erlipidemic and antiatherogenic activities. These activities of the compositions further contribute to health, wellness, healthy ageing, and longevity'.
  • Various embodiments disclosed herein relate to a combination of two natural products for decreasing craving, reducing appetite, enhancing satiety, and stress reduction and mood improvement, containing an extract of Cyper s escukntus and Mangiferin.
  • the combination has an effect comparable to the appetite-reducing effect provided by either Rimonabant or Methylphenidate, but does not possess the negative drawbacks of these drugs.
  • it has the capacity to enhance mood and reduce stress, as opposed to the increase in stress and low mood or depression commonly associated with weight-loss and smoke-cessation programs, and with the relapses seen commonly after completion of such programs.
  • This combination is based on functional foods and is not addictive. It can be combined with numerous natural compounds or plant extracts for additional benefits or flavoring or can be added into existing formats, formulations and food products in several ways, being for example a liquid or a powder, granules, a gum or a sachet.
  • the ingredients of the described invention are a water or ethanolic extract of whole Tigernut or Tigernut peel, and pure mangiferin or a plant extract standardized to mangiferin, derived by extraction of, for example, mango leaves, mango bark, mango fruit, or honey bush tea. These products can form part of different products and can be combined in different ratios and added to other ingredients.
  • Various embodiments disclosed herein relate to methods for reducing craving, reducing appetite, and enhancing satiety to avoid weight-gain and relapse after smoking- cessation, improve mood and reduce stress and depression in a person in need thereof, by administering an herbal composition to said person.
  • the herbal composition may comprise an effective amount of an extract of Cyperus escukntus peel, Cperus escukntus rhizomes, or a combination thereof.
  • the herbal composition may comprise an effective amount of mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol.
  • the herbal composition may comprise a mixture of an effective amount of an extract of Cjperus escukntus peel, Cjperus escukntus rhizomes, or a combination thereof; and an effective amount of mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol.
  • the extract of Cjperus escukntus peel and/or Cjperus escukntus rhizomes, or a combination thereof is an aqueous extract, an alcoholic extract, or a hydroalcoholic extract.
  • the extract of Cjperus escukntus may be a hydroalcoholic extract of peel of Cyperus esculentus rhizomes.
  • the extract of Cjperus escukntus peel and/ or Cjperus escukntus rhizomes may be used in an amount of between 20 mg and 20 g per dose.
  • the herbal composition contains mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol, used in an amount of between 20 mg and 5 g per dose. In some embodiments, the herbal composition contains an extract comprising mangiferin or norathyriol in an amount sufficient to provide between 20 mg and 5 g mangiferin or norathyriol per dose.
  • the extract comprising mangiferin or norathyriol may be a mangiferin-containing extract of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, Coffea, and mixtures thereof.
  • Various embodiments disclosed herein relate to methods for reducing craving, reducing appetite, enhancing satiety, reducing stress and enhancing mood in a person or animal in need thereof, by administering a herbal composition to said person, by administering a mixture of an effective amount of:
  • the effective amount of (a) is between 20 mg and 20 g per dose; and the effective amount of said mangiferin or said mangiferin-containing extract is between 5 mg and 5 g per dose.
  • the mixture of (a) and (b) is provided as a unit dose containing between about 10 mg and about 20 g per dose.
  • the herbal compositions disclosed herein contain:
  • a) a herbal composition comprising:
  • an active ingredient to support weight management or smoking cessation activity selected from the group consisting of 5-hydroxytryptophan, B group vitamins, caffeine, celastrol, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin, doco sah exaeno i c acid, eicosapentaenoic acid, ginsenosides, glycomacropeptide, huperzine, hydrocycitrate, L-carnitine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N-methyltyramine, oleamide, omega-3 fatty acids, octopamine, phenylalanine, phenylethylamine, phosphatidlyserine, phosphatidlyserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine,
  • compositions and methods for reducing craving, reducing appetite, enhancing satiety while elevating mood, treating depression, and decreasing stress are common side effects of pharmaceuticals for reducing appetite and increasing satiety.
  • the method comprises replacement of drugs for satiety and appetite reduction with a product of the composition comprising:
  • Various embodiments disclosed herein relate to methods for reducing craving, reducing appetite, enhancing satiety while enhancing mood and decreasing stress, preventing weight gain during and subsequent to smoking cessation, during responsible calorie restriction diets for maintaining health, facilitating healthy ageing and longevity of a composition
  • a composition comprising:
  • an effective amount of mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol where the effective amount may be between about 10 mg and about 500 mg, between about 10 mg and about 350 mg, between about 10 and about 200 mg, between about 5 and about
  • Cjperus escukntus and mangiferin can be used to reduce craving , reduce appetite, and enhance satiety alone or in combination with a weight loss product or program or a smoking cessation program.
  • Both extracts are anticipated, through their mood-activating effect to have mood-enhancing and anti-depressant activities comparable to Selegiline and other antidepressants.
  • These extracts are expected to reduce craving as effectively as Rimonabant or Methylphenidate.
  • these natural functional food extracts have been demonstrated to lack the undesirable side effects associated with the Rimonabant and Methylphenidate.
  • the combination of Cperus escukntus and mangiferin has an EEG signature that is comparable to that of the pharmaceutical selegiline, which has an anti-depressant effect.
  • the EEG signature in rats shows synergy for alpha- 1 brain wave attenuation in vivo from implanted electrodes in rats, which indicates synergy of the composition for enhancing mood / treating depression, and decreasing stress.
  • composition comprises:
  • composition When the composition is administered to a person attempting to quit smoking, the composition is administered in an amount effective to reduce at least one of theta brain wave activity and an alpha-l/alpha-2 ratio in the person.
  • composition When the composition is administered to a person attempting to reduce caloric intake, the composition is administered in an amount effective to reduce cravings for food by reducing beta brain wave activity in the person.
  • composition When the composition is administered to a person attempting to quit smoking, the composition may be administered in an amount effective to:
  • composition comprises:
  • composition is administered in an amount effective to modulate alpha brain wave activity in said person.
  • the person is subject to stress from attempts to lose weight, control food intake, or stop smoking.
  • the Cyperus esculentus extract/mangiferin composition helps relieve this stress by modulating alpha brain wave activity. Reduced stress may avoid relapses into eating or smoking.
  • compositions for reducing craving and improving mood and depression/ stress in a person in need thereof, comprising administering a composition to said person, where the composition comprises:
  • a person in need thereof refers to any person or human subject in need of craving reduction to support a weight management or anti-smoking program or in need of a mood enhancer and anti-depressant.
  • Such personor human subjects may be children, adolescents, adults, or elderly persons.
  • Such personor human subjects may be people with overweight, obesity or smokers in need of reduced craving while avoiding depression or improving their mood during and after a weight-loss or smoking-cessation program, thereby increasing adherence and reducing risk of relapse.
  • Various embodiments disclosed herein relate to herbal compositions for reducing craving and improving mood, comprising an effective amount of an extract of Cyperus esculentus.
  • the extract of Cyperus esculentus may be an extract of the entire plant, or of any plant part.
  • the plant part of Cyperus esculentus to be extracted may be the leaf, peel, root, rhizome, stem, tuber, or a combination thereof.
  • the extract of Cyperus esculentus may be an extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, a peel derived from Cyperus esculentus rhizomes, or a combination thereof.
  • the plant part of Cyperus esculentus may be extracted with water, an organic solvent, or a mixture thereof.
  • the organic extraction solvent may be a polar aprotic solvent, such as DMSO, acetone, or a mixture thereof; or a polar protic solvent, such as a lower alcohol having from 1 to 4 carbon atoms.
  • the extract of Cyperus esculentus is an extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, a peel derived from Cyperus esculentus rhizomes, or a combination thereof, derived by extraction with water, a lower alcohol having from 1 to 4 carbon atoms, or a mixture thereof.
  • the extract of Cyperus esculentus is an extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, a peel derived from Cyperus esculentus rhizomes, derived by extraction with a hydroalcoholic mixture of water and ethanol.
  • the extract may be obtained from extraction by subcritical or supercritical C02.
  • Mangiferin has a structure of formula la, where R is a 1,5-anhydro-D-glucitol ring.
  • Norathyriol is an aglycone of mangiferin, and has a structure of formula lb, where R is hydroxyl.
  • mangiferin is here defined as encompassing:
  • mangiferin as a pure compound, where "pure” is defined as meaning the compound is at least 90% mangiferin, at least 95% mangiferin, at least 98% mangiferin, or at least 99.5% mangiferin; or
  • composition comprising at least 90% by weight of a mixture of mangiferin and norathyriol.
  • Mangiferin is a xanthonoid polyphenol. Mangiferin is found in several botanicals, including extracts of mango fruit, mango peel, mango bark, and/ or mango leaf, as well as in extracts of various Cyclopia species, e.g., Honeybush tea, and extracts of species in the genus Salacia. Mangiferin has acetyl choUnesterase inhibiting activity, an activity useful in improving cognitive function in Alzheimer's disease.
  • Mangiferin a xanthonoid
  • Mangiferin is a natural phenolic compound formed from the xanfhone backbone. If we refer to Mangiferin, its aglycone norathyriol is always included as an alternative ingredient.
  • Mangiferin is an antioxidant and anti-inflammatory that exhibits various pharmacological activities, including anti-diabetic, anti-cancer, and anti-oxidant effects as well as anti-inflammatory, anti-viral, immunomodulatory and anti-microbial activities.
  • Mangiferin may play a role in pathologies related to neuroinflammation and oxidative damage. Mangiferin may also enhance recognition memoir) ' and improve memory deficits, while the inhibition of MAO A seems to be responsible for its anti-depressant-like effect. No effects indicating a reduction of craving have been described in the literature
  • Mangiferin of the invention may be extracted from a plant containing Mangiferin.
  • Excellent sources of the desired material are Mangifera indica (fruit, bark or leaf) or Honey bush tea, which are preferably standardized to a concentration of 20-70% Mangiferin, depending on the raw material.
  • mangiferin can be obtained from other sources, including plant species of the genera Mangifera, Salacia, Cyclopia, Hypericum, Mangifera, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and Coffea.
  • Tigernut (Cperus escukntus), a crop of the sedge family widespread across the world, is a typical Spanish food found on markets and in the supermarket. In Spain, the milky extract of Tigernut (i.e., "horchata de chufa"), a non-alcoholic beverage, has an annual economic impact of 60 million Euro. Tigernut is rich in fiber, proteins, sugars, oleic acid and glucose, as well as in phosphorus, potassium, and vitamins C and E. Tigernut is useful for enhancing blood circulation, preventing heart disease, and reducing the risk of colon cancer. The scientific literature has not described any effect of chufa toward reduction of cravings, e.g., cravings for food or tobacco, or improvement of mood.
  • the combination of Tigernut and Mangiferin serves to moderate the bitter taste and unusual flavor of Mangiferin.
  • the electropharmacogram of the combination is strikingly similar to the electropharmacograms of Rimonabant and Methylphenidate (Ritalin), both appetite inhibitors, and Selegiline (an an antidepressant drug and anti- Parkinson's drug successfully used for smoking-cessation and as anti-depressant) (Fig. 1).
  • the invention resulted in a synergistic attenuation of Hippocampus alpha 1 and alpha 2 brain waves in rats (Fig 2D), representing an activation of the neurotransmitters serotonin and dopamine, which are closely related to the reward system and the homeostasis of regulation of food intake.
  • Mangiferin and its aglycone metabolite norathyriol may be included in the disclosed compositions as pure compounds, or as components of an extract of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, Coffea and mixtures thereof.
  • the plant species contain mangiferin and/or norathyriol, and may be extracted with water, an aqueous base, a polar protic organic solvent, a polar aprotic organic solvent, or a mixture thereof.
  • the plant species comprises mangiferin, and is extracted with water, a lower alcohol having 1 to 4 carbon atoms, or a mixture thereof.
  • the herbal composition contains mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol, used in an amount of between 20 mg and 5 g per dose.
  • the herbal composition may contain an extract comprising mangiferin or norathyriol of between 20 mg and 5 g per dose. If the concentration of mangiferin and/ or norathyriol in the extract is known, the extract may be provided in an amount sufficient to provide between 20 mg and 5 g mangiferin or norathyriol per dose.
  • an extract of a plant of the genus Mangifera contains 30% mangiferin
  • the extract may be provided in an amount of between 20 mg and 5 g per dose, based on the weight of the extract.
  • the Mangifera extract may be administered in an amount of between 66.7 mg and 16.7 grams per dose, so as to provide between 20 mg and 5 g mangiferin per dose.
  • compositions containing Chufa or Tigernut extracts and mangiferin-containing botanical extracts where the compositions are effective in enhancing CNS activity in the frontal cortex, hippocampus and striatum.
  • the compositions are effective for reduction of cravings, as shown by increased alpha wave activity in the brain.
  • the compositions are also effective for improving mood and reducing depression, as shown by the similarity to Selegiline and the increased release of Serotonin, indicated by reduction of alpha- 1 waves in rat EEG.
  • Cjperus escukntus extracts and mangiferin have a very similar CNS activating effect (as evidenced by EEG) to each other and to Rimonabant, Methylphenidate and Selegiline.
  • Cjperus escukntus extracts and mangiferin also exhibit a calming, de-stressing activity when ingested.
  • Cperus escukntus extracts and mangiferin exhibit a plateau effect. Beyond a certain threshold value, an increased intake of these extracts does not give greater CNS stimulation, minimizing abuse potential.
  • Cjperus escukntus extracts and mangiferin exhibit none of the well-known side effects, e.g., sleeplessness and depression, caused by excessive doses of Rimonabant or Methylphenidate.
  • Chufa peels have, in the prior art, generally been considered to be a waste product of Chufa processing. However, it has been discovered that a 30% ethanol-water extract of chufa peels, e.g., peels of Chufa tuberous rhizomes, exhibit more potent activating activity than a 30% ethanol-water extract of whole chufa, which in turn has more potent activity than a water extract of whole chufa. Ethanolic, aqueous, and hydroalcoholic extracts of Chufa tuberous rhizomes all, however, exhibit desirable CNS activating activity.
  • Chufa or Tigernut extracts and mangiferin-containing botanical extracts may be taken as individual active ingredients.
  • Chufa or Tigernut extracts are desirably taken by an adult human in an amount of about 0.1 g/ day to about 10 g/ day, about 0.5 g/day to about 8 g/day, about 1 g/day to about 5 g/day, or about 1 g/day to about 4 g/day.
  • Mangiferin-containing botanical extracts are desirably taken by an adult human in an amount of about 25 mg/day to about 5 g/day, about 50 mg/day to about 2 g/ day, about 100 mg/ day to about 1 g/ day, or about 200 mg/ day to about 400 mg/ day.
  • Chufa or Tigernut extracts and mangiferin-containing botanical extracts have synergistic activity on alpha-1 and alpha-2 brain wave activity in the hippocampus.
  • Chufa or Tigernut extracts and mangiferin-containing botanical extracts are desirably combined in a ratio of between about 0.5:1 and about 30:1, about 1:1 and about 20:1, about 5:1 and about 10:1 and about 7.5:1.
  • the herbal compositions disclosed herein contain a herbal composition comprising:
  • mangiferin an effective amount of mangiferin or an extract comprising mangiferin; or a mixture of an extract of Cyperus esculentus peel or rhizomes and mangiferin or an extract comprising mangiferin.
  • compositions may comprise:
  • Hi from about 10% to about 95% by weight, about 25% to about 90% by weight, about 40% to about 85% by weight, or about 50% to about 80% by weight, of a mixture of
  • an extract of Cyperus esculentus peel and/ or rhizomes and b. mangiferin or an extract comprising mangiferin; and from about 5% to about 90% by weight, about 10% to about 75% by weight, about 15% to about 60% by weight, or about 20% to about 50% by weight of the further ingredient for enhancing mood or decreasing stress or anxiety.
  • This further ingredient for further enhancing mood or decreasing depression, stress or anxiety is selected from the group consisting of 5- hydroxytryptophan, B group vitamins, caffeine, citicoHne, citrulHne, choHne, chromium picolinate, coenzyme Q10, curcumin, glycomacropeptide, huperzine, hydrocycitrate, L-carnitine, L-carnosine, L-tryptophan, luteoHn, ibogaine, magnesium, N-methyltyramine, oleamide, omega-3 fatty acids, octopamine, phenylalanine, phenylethylamine, phosphatidlyserine, phosphatidlyserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine, xanthohumol, yangonin, yohimbine, e
  • Mangiferin and Mangifera extracts may be incorporated into an oral dosage form, including an orally dissolvable or dispersible buccal strip, a chewing gum, a tablet, a capsule, an emulsion, a suspension, an oral spray, effervescent, dissolvable granules or powder, a sachet, or a clear beverage.
  • Chufa extracts are typically opaque and milky in beverage form, and may be incorporated into an oral dosage form, including an orally dissolvable or dispersible buccal strip, a chewing gum, a tablet, a capsule, dissolvable granules or powder, a sachet, an emulsion, a suspension, dairy milk, non-dairy milks, yoghurt, and milk-fruit juice combinations.
  • compositions disclosed herein may be provided as:
  • an orally dissolvable or dispersible buccal strip for mucosal absorption, a chewing gum, a chewable tablet, a lozenge, an effervescent tablet, a capsule, or an emulsion; a functional chocolate, marzipan, or sweetmeat,
  • compositions disclosed herein may be used for anti-craving reasons in weight control programs of for smoking cessation and may be added to all kind of formats, replacing pharmaceuticals currently used for appetite reduction or satiety.
  • Rimonabant Removing all or part of the pharmaceutical drug in a product with an extract of Cyperus esculentus peel and/or rhizomes, mangiferin or an extract comprising mangiferin, or a mixture thereof allows the side effects of this drug (for example Rimonabant) to be removed, while restoring the desired CNS stimulant activity. It is estimated that about 2 grams chufa extract is equivalent to 10 mg Rimonabant or lOmg Methylphenidate. Similarly, Mangiferin and mangiferin-containing extracts may be used to reduce craving in a food, beverage or supplement. It is estimated that about 100 to about 200 mg mangiferin is equivalent to lOmg Rimonabant or lOmg Methylphenidate.
  • a composition combining Cyperus esculentus extract and Mangiferin in a ratio of between about 20:1 and 1:1 may be used instead of 10 mg Rimonabant or lOmg Methylphenidate. From about 20 mg to about 200 mg of the Cyperus esculentus extract/Mangiferin combination may be used to replace lOmg mg of Rimonabant or lOmg Methylphenidate.
  • the combined Cyperus esculentus-mangiferin or mangiferin containing plant extract is used in an amount of between lOmg and 20g for Rimonabant or Methylphenidate substitution.
  • the Cyperus esculentus extract/Mangiferin composition in accordance with the invention may be a simple mixture of the two ingredients after the extraction process.
  • the invention may advantageously include additional ingredients with the purpose to further increase the craving reducing effect and the positive effect on weight loss or smoking cessation. Therefore, it may be advantageous to add, for example, other appetite reducing, mood improving, anti-obesity, or anti-craving components to the combined product presented, to enhance the anti-craving effect provided by the present invention.
  • the same products can also be added to Cyperus esculentus extract or Mangiferin separately.
  • natural products like Ganoderma, Garcinia Kola and Astragalus can be combined with the composition.
  • Ingredients enhancing absorption and bioavailability may be added, like Piperin, Capsaicin or Ginger.
  • Natural and artificial sweeteners, and flavors such as coffee, vanilla, hazelnut, chocolate, cream, or fruit flavor can be integrated.
  • Nutrients like omega-3 fatty acids, vitamins and minerals may be added.
  • antioxidants include polyphenols with anti-oxidant or xanthin-oxidase inhibitory effects can be added.
  • Representative polyphenols include catechins from Green tea, polyphenols from Cocoa, resveratrol from grape, Polygonum or Gnetum gnemon seeds, xanthohumol from Humulus lupulus, and luteolin, rutin or quercetin.
  • the Cyperus esculentus extract/Mangiferin composition may be combined with anti-craving, weightloss or anti-smoking products such as Hoodia, Curcuma and Ginger, and/ or mood improving-products such as Ginkgo, citicoline or huperzine.
  • the amount of the additional ingredient included in the in the composition of the present invention varies depending on the characteristics of each additional ingredient.
  • the invention can be combined, for example, with an anti-oxidant in a ratio from 1:50 to 50:1.
  • the composition has a wide range of useful applications for the industry: it can be provided in a liquid, syrup, or solid (tablet) or pulverized or granulated or gum form or can be incorporated into food products of liquid, solid (tablet), syrup granulated or pulverized consistency.
  • the liquid may be presented in a concentrated form to be diluted by mixing it with teas, coffee, water or milk, juices, yoghurts or smoothies to provide the final consumable liquid beverage providing the craving reduction typically associated with Rimonabant and the mood enhancing benefits.
  • the concentration of the present invention varies depending on the product format, purpose and/ or the additional ingredients.
  • compositions disclosed herein may be used for replacing pharmaceuticals currently used for appetite reduction or satiety, notably Rimonabant and Methylphenidate.
  • pharmaceuticals currently used for appetite reduction or satiety notably Rimonabant and Methylphenidate.
  • about 2 to 5 grams Cyperus esculentus extract has an activity which is equivalent to 5.5 to 14.5 mg Rimonabant or 5.5 to 14.5 mg Methylphenidate; about 3 to 4 grams Cyperus esculentus extract has an activity which is equivalent to 8.5 to 11.5 mg Rimonabant or 8.5 to 11.5 mg Methylphenidate; or about 3.5 grams Cyperus esculentus extract has an activity which is equivalent to 10 mg Rimonabant or 10 mg Methylphenidate.
  • mangiferin is equivalent to about 10 to 40 mg Rimonabant or about 2 to 8 mg Methylphenidate
  • about 200 to about 300 mg mangiferin is equivalent to about 20 to 30 mg Rimonabant or about 4 to 6 mg Methylphenidate
  • about 250 mg mangiferin is equivalent to about 25 mg Rimonabant or 5 mg Methylphenidate.
  • a composition combining Cyperus esculentus extract and Mangiferin in a ratio of between about 20:1 and 1:1 may be used for reduction of cravings. From about 20 mg to about 200 mg of the Cyperus esculentus extract/Mangiferin combination may be used to replace 5 mg to 50 mg Rimonabant or 1 to 10 mg Methylphenidate; or about 100 mg of the Cyperus esculentus extract/Mangiferin combination may be used to replace 25 mg Rimonabant or 5 mg Methylphenidate.
  • the combined Cyperus esculentus-mangiferin or mangiferin containing plant extract can be used in an amount of between lOmg and 20g for replacing lOmg Rimonabant or lOmg Methylphenidate substitution.
  • composition of the invention can also be a pharmaceutical composition, further comprising a pharmaceutically acceptable excipient.
  • pharmaceutically acceptable excipients include water, an alcohol such as ethanol or mixtures therefrom.
  • Embodiment 1 A composition comprising:
  • Embodiment 2 The composition for use according to Embodiment 1, wherein said person is attempting to quit smoking; and said composition reduces cravings for nicotine-containing products in said person.
  • Embodiment 3 The composition for use according to Embodiment 1 or Embodiment 2, wherein said composition is administered in an amount effective to reduce theta brain wave activity and alpha-l/alpha-2 ratio in said person.
  • Embodiment 4 The composition for use according to Embodiment 1, wherein said person is attempting to reduce caloric intake; and said composition reduces cravings for food in said person; wherein said composition is administered in an amount effective to reduce beta brain wave activity in said person.
  • Embodiment 5 The composition for use according to Embodiment 3, wherein said composition further reduces cravings for food in said person; wherein said composition is administered in an amount effective to reduce theta brain wave activity, beta brain wave activity, and alpha-l/alpha-2 ratio in said person.
  • Embodiment 6 A composition comprising:
  • composition for use in the reduction of stress and improving mood in a human person, wherein said composition modulates alpha brain wave activity in said person.
  • Embodiment 7 The composition for use according to any one of Embodiments 1 to 5, wherein said composition comprises said extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, or a combination thereof.
  • Embodiment 8 The composition for use according to any one of Embodiments 1 to 5 or 7, wherein said extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, or a combination thereof is an aqueous extract, an alcoholic extract, or a hydroalcoholic extract, or a subcritical or supercritical C02 extract.
  • Embodiment 9 The composition for use according to any one of Embodiments 1 to 5 or Embodiments 7 or 8, wherein said extract composition comprises a hydroalcoholic extract of peel of Cyperus esculentus rhizomes.
  • Embodiment 10 The composition for use according to any one of Embodiments 1 to 5, or Embodiments 7 to 9, wherein said effective amount of said Cyperus esculentus peel, Cyperus esculentus rhizomes, or a combination thereof is between 20 mg and 20 g per dose.
  • Embodiment 11 The composition for use according to any one of Embodiments 1 to 5, wherein said composition comprises said effective amount of mangiferin, norathyriol, or an extract comprising mangiferin or norathyriol.
  • Embodiment 12 The composition for use according to Embodiment 11, wherein said effective amount of said mangiferin or said norathyriol is between 20 mg and 5 g per dose.
  • Embodiment 13 The composition for use according to Embodiment 11, wherein said effective amount of said extract comprising mangiferin or norathyriol is sufficient to provide between 20 mg and 5 g mangiferin or norathyriol per dose.
  • Embodiment 14 The composition for use according to any one of Embodiments 1 to 5, or Embodiments 11 to 13, wherein said extract comprising mangiferin or norathyriol is a mangiferin-containing extract of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
  • Embodiment 15 The composition for use according to any one of Embodiments 1 to 5, wherein said composition comprises said synergistic combination of (a) and (b).
  • Embodiment 16 The composition for use according to Embodiment 15, wherein (a) is an aqueous extract, an alcoholic extract, or a hydroalcoholic extract of Cyperus esculentus peel, Cyperus esculentus rhizomes, or a combination thereof.
  • Embodiment 17 The composition for use according to any one of Embodiments 15 or 16, wherein (a) comprises a hydroalcoholic extract of peel of Cyperus esculentus rhizomes.
  • Embodiment 18 The composition for use according to any one of Embodiments 15 to 17, wherein (b) comprises mangiferin or a mangiferin-containing extract of a plant species in a genus selected from the group consisting of Mangifera, Salacia, Cyclopia, Hypericum, Canscora, Fagraea, Gentiana, Hoppea, Swertia, Hypericum, Polygala, Zizyphus, and mixtures thereof.
  • Embodiment 19 The composition for use according to any one of Embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 1:1 and about 50:1.
  • Embodiment 20 The composition for use according to any one of Embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 1:1 and about 20:1.
  • Embodiment 21 The composition for use according to any one of Embodiments 15 to 18, wherein the ratio of (a) to (b) is between about 4:1 and about 15:1.
  • Embodiment 22 The composition for use according to Embodiment 18, wherein said effective amount of (a) is between 20 mg and 20 g per dose; and said effective amount of said mangiferin or said mangiferin-containing extract is between 5 mg and 5 g per dose.
  • Embodiment 23 The composition for use according to any one of Embodiments 15 to 19, wherein said composition is provided as a unit dose containing between 10 mg and 20 g per dose.
  • Embodiment 24 The composition for use according to any one of Embodiments 1 to 5 or 7 to 23 or the composition for use according to Embodiment 6, wherein said composition further comprises an active ingredient selected from the group consisting of 5-hydroxytryptophan, B group vitamins, caffeine, citicoline, citrulline, choline, chromium picolinate, coenzyme Q10, curcumin, glycomacropeptide, huperzine, hydrocycitrate, L-carnitine, L-carnosine, L-tryptophan, luteolin, ibogaine, magnesium, N- methyltyramine, oleamide, omega-3 fatty acids, octopamine, phenylalanine, phenylethylamine, phosphatidlyserine, phosphatidlyserine, quercetin, raspberry ketones, rutin, resveratrol, synephrine, taurine, taxifoline, theanine, theobromine
  • Embodiment 25 A composition comprising:
  • Embodiment 26 A pharmaceutical composition comprising a composition for use according to Embodiment 1, or a composition for use according to Embodiment 6, or a composition for use according to Embodiment 25, further comprising a pharmaceutically acceptable excipient.
  • Test Subjects Fisher 344 rats (11 months of age and day - night converted, weight about 350 - 400 g, provided by Charles River Laboratories, D-97633, Sulzfeld) were used in a series of experiments on the effects of various herbal and pharmaceutical products on central nervous system activity. Products were provided to the test subjects orally (gavage).
  • Test Substances The substances tested in this study included:
  • a control vehicle (0.9% NaCl);
  • Mango leaf ethanol extract, administered in an amount of 50 mg/kg to 7 rats;
  • Cyperus Esculentus tuberous rhizome peel ethanol extract, 150mg/kg, plus Mango leaf extract, containing 60% of Mangiferin, 50mg/kg, administered to 5 rats
  • Selegiline administered in amount of l,5mg/kg to 8 rats
  • EEG signals were recorded by telemetry from 4 implanted electrodes in the frontal cortex, hippocampus and striatum of freely moving rats from inside a totally copper shielded room. Signals were collected in sweeps of 4-second duration and Fast Fourier transformed using a Hanning window. EEG signals were recorded over a period starting 5 minutes after administration of the test substances, and ending 65 minutes after administration of the test substances. Sampling frequency was 512 Hz. Spectra were averaged in steps of 3 minutes each and displayed on-line. In an off-line procedure, the spectra were averaged to give longer periods for further analysis and data presentation. Spectral activity within the frontal cortex, hippocampus, striatum and reticular formation was recorded. Oral administration of the control vehicle (0.9% NaCl) only resulted in minor changes of spectral power within the four brain areas.
  • a control vehicle (0.9% NaCl);
  • Mango leaf extract containing 60% Mangiferin administered in an amount of 50 mg/kg to 6 rats; and a mixture of Cyperus esculentus tuberous rhizome peel, 30% ethanol extract, in an amount of 150 mg/kg, and Mango leaf extract containing 60% Mangiferin, in an amount of 50 mg/kg, the combination being administered to 6 rats.
  • EEG signals were recorded by telemetry from 4 implanted electrodes in the frontal cortex, hippocampus and striatum of freely moving rats from inside a totally copper shielded room. EEG signals were recorded over:
  • Mango leaf extract containing 60% Mangiferin also decreased brain wave activity in the frontal cortex.
  • brain wave activity in both the frontal cortex and the hippocampus from delta, theta, alpha-2, and beta-1 waves decreased noticeably, as shown in FIG. 2C.
  • the decrease in delta and theta wave activity was statistically significant (p ⁇ 0.05).
  • brain wave activity in the hippocampus from theta, alpha- 1, and alpha-2 waves decreased significantly (p ⁇ 0.05 for alpha- 1 and alpha-2 waves; p ⁇ 0.1 for theta waves).
  • the combination of the Cyperus esculentus and the Mango leaf extract produced a statistically significant (p ⁇ 0.05) increase in gamma wave activity in the frontal cortex. Increased gamma-band EEG activity is associated with states of alertness or attention.
  • the combination of Cyperus esculentus extract and the Mango leaf extract has a statistically significant impact on alpha-1 brain wave activity in the hippocampus, both in the first hour after administration and 5 hours after administration (p ⁇ 0.05, both 1 hour after administration and 5 hours after administration). Further, neither the Cyperus esculentus extract nor the Mango leaf extract has any statistically significant impact on brain wave activity in the hippocampus 5 hours after administration, as shown in FIGS. 2B and 2C. The combination of Cyperus esculentus extract and the Mango leaf extract has a synergistic, statistically significant impact on alpha-brain wave activity in the hippocampus 5 hours after administration, related to an increase of serotonergic activity.
  • the Profile of Mood States is a psychological rating scale used to assess transient, distinct mood states.
  • the assessment provides a rapid method of assessing transient, fluctuating active mood states. It is an instrument for measuring and monitoring treatment change in clinical, medical, and addiction treatment centers. It is also well suited to clinical drug trials because its sensitivity to change allows accurate documentation of the effects of drugs on mood state.
  • POMS is a standard validated psychological test containing 65 words or statements describing feelings that people have. The test requires an indication, for each word or statement, how the subject has been feeling in the previous week, Possible scores for each word or statement include:

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Abstract

L'invention concerne une méthode pour améliorer au moins l'un des points suivants : la réduction de l'état de manque, l'amélioration de l'humeur, l'évitement de la dépression, la prévention du gain de poids après une perte de poids suite à un régime, la réduction des effets secondaires négatifs produits par des médicaments coupe-faim et l'arrêt de fumer et la promotion du vieillissement sain chez une personne qui en a besoin, comprenant l'administration d'une composition à ladite personne, ladite composition comprenant : a) une quantité efficace d'un extrait d'écorce de Cyperus esculentus, de rhizomes de Cyperus esculentus ou d'une combinaison de ceux-ci; b) une quantité efficace de mangiférine, de norathyriol, ou d'un extrait comprenant de la mangiférine ou du norathyriol; ou c) une combinaison synergique de (a) et (b). La composition peut comprendre un troisième ingrédient actif en combinaison avec l'extrait de Cyperus esculentus et la mangiférine ou le norathyriol.
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CN110292547B (zh) * 2019-08-08 2022-03-11 广东丸美生物技术股份有限公司 化妆品组合物及其制备方法和具有抗蓝光作用的化妆品
CN111466908B (zh) * 2020-04-09 2022-08-09 瘦声(杭州)科技有限公司 一种利用eeg筛选可影响食欲音频的方法
KR102282491B1 (ko) * 2020-10-26 2021-07-27 주식회사 에스앤케이바이오텍 탄수화물 함량이 저감된 탄수화물 음식의 제조방법
KR102269586B1 (ko) * 2020-11-10 2021-06-24 농업회사법인 주식회사 오케이120 식욕 조절 및 체중 감량 목적의 다이어트용 사탕
JP2022097984A (ja) * 2020-12-21 2022-07-01 富士フイルム株式会社 精神状態改善剤
KR102255693B1 (ko) 2021-02-22 2021-05-25 주식회사 인화무역 시서스의 재배방법
JP2024509922A (ja) * 2021-03-09 2024-03-05 ニコベンチャーズ トレーディング リミテッド 経口製品及び製造の方法
CN113341050B (zh) * 2021-04-28 2023-05-02 内蒙古大学 一种油莎草地上部分多种成分的液质定量方法及其应用
CN115137066A (zh) * 2022-05-31 2022-10-04 澳美制药(苏州)有限公司 一种减肥片剂及其制备方法
AU2023311967A1 (en) * 2022-07-19 2025-02-06 Pinata Holdings Inc. Inhalable serotonin receptor agonist formulations

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100663181B1 (ko) * 2004-10-19 2007-01-02 대구한의대학교산학협력단 니코틴 중독 및 금단증상의 예방 및 치료를 위한 산조인 추출물을 함유하는 조성물
EP3009138B1 (fr) * 2014-09-01 2019-05-01 Shyam Prasad Kodimule Extrait de mangifera pour la gestion de l'obésité et/ou du poids

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2082170B (en) 1980-07-16 1984-03-28 Vnii Lekarstvenny Process for preparing mangiferin
US4436732A (en) 1981-10-26 1984-03-13 Vichkanova Serafima A Medicated compound for treating diseases infected by virus of the herpes group
ES2111500B1 (es) 1996-08-22 1998-07-16 Coret Monros Salvador Proceso para la obtencion de una composicion alimenticia a base de chufa y platano.
US5985282A (en) 1997-01-22 1999-11-16 Hpf, L.L.C. Herbal appetite suppressant and weight loss composition
US5798101A (en) * 1997-01-22 1998-08-25 Hpf, L.L.C. Herbal appetite suppressant and weight loss composition
AU774700B2 (en) 1999-11-12 2004-07-01 K.M. Slimak Use of tropical root crops in effective intervention strategies for treating difficult and complex cases and chronic diseases
US6613797B2 (en) 1999-12-02 2003-09-02 Interlab, Inc. Xanthone analogs for treating infectious diseases and complexation of heme and porphyrins
RU2176516C1 (ru) 2000-11-17 2001-12-10 Чернов Юрий Николаевич Адаптоген стресс-корректор
RU2197259C1 (ru) 2001-07-18 2003-01-27 Чернов Юрий Николаевич Антидиабетическое средство
ES2277567B1 (es) * 2005-12-30 2008-06-01 Universidad Del Pais Vasco Compuestos con propiedades neuroprotectoras.
CN101003558A (zh) 2006-10-17 2007-07-25 中国人民解放军第二军医大学 芒果苷类化合物以及其制备方法和在医药领域的应用
WO2008061480A1 (fr) 2006-11-24 2008-05-29 Hainan Deze Drug Research Co., Ltd Nouveaux sels de calcium de mangiférine, leur procédé de preparation et leur utilisation
CN101848922B (zh) 2007-11-22 2013-01-02 海南德泽药物研究有限公司 一种新的芒果苷钙盐及其制备方法与用途
EP2220103B1 (fr) 2007-11-22 2015-04-08 Hainan Deze Drug Research Co., Ltd Nouveaux sels de calcium de mangiférine, leur procédé de préparation et leur utilisation
FR2926726B1 (fr) 2008-01-28 2010-04-02 Limousine D Applic Biolog Dite Utilisation d'un actif issu de cyperus esculentus pour son action anti-age.
FR2929945B1 (fr) 2008-04-11 2010-09-03 Inst Rech Developpement Ird Procede d'extraction de mangiferine et d'isomanfigerine.
CN101270230B (zh) 2008-05-20 2012-06-20 贺州学院 一种超声波辅助提取荸荠皮天然棕色素的方法
CN101269161B (zh) 2008-05-20 2011-12-07 贺州学院 一种从荸荠皮中提取总黄酮的工艺
GB2464700B (en) 2008-10-22 2012-11-28 Univ Plymouth A method of colouring tin and tin-containing articles
CN101732360B (zh) 2008-11-14 2011-09-07 郑州豫密药业股份有限公司 中药丸剂的打光方法
CN101921270A (zh) 2009-06-16 2010-12-22 海南德泽药物研究有限公司 一种芒果苷小檗碱盐及其制备方法与用途
CN101731710B (zh) 2010-01-17 2012-11-28 李国平 一种油莎豆饮料及其制作方法
EP2397039A1 (fr) * 2010-06-21 2011-12-21 Abbott Laboratories Compositions destinée à retarder la progression du diabète utilisant un extrait de Salacia oblonga
CN103191141B (zh) 2012-01-05 2014-10-22 昆明制药集团股份有限公司 3-甲氧基芒果苷在制备治疗脑卒中后抑郁药物中的应用
US9198943B2 (en) * 2012-07-12 2015-12-01 Michael Parker Jones Silene capensis for inhibiting cravings
CN102920696B (zh) 2012-09-27 2015-03-18 戴好富 芒果苷类化合物或芒果提取物用作胰脂肪酶抑制剂、制备防治肥胖的药物或食品的应用
US20140220220A1 (en) 2013-02-05 2014-08-07 Nutso, Llc Tiger nut foodstuff and systems and methods for processing tiger nut foodstuffs
CN104557892B (zh) 2013-10-14 2018-01-02 北京大学 一种芒果苷单位点衍生物及其制备方法和用途
TW201609123A (zh) * 2013-11-19 2016-03-16 歐姆尼艾克提夫健康科技（加拿大）有限公司 五層龍屬組成物、藉由其投藥之治療方法及其製備方法
CN103877014A (zh) * 2014-03-26 2014-06-25 邓家刚 一种芒果苷口服液及其制备方法
CN104083571B (zh) * 2014-07-29 2017-03-29 新疆大学 一种有增强微循环作用的油莎草总黄酮的提取方法及应用
US10537604B2 (en) 2016-07-19 2020-01-21 Nektium Pharma, S.L. Compositions for enhancing brain activity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100663181B1 (ko) * 2004-10-19 2007-01-02 대구한의대학교산학협력단 니코틴 중독 및 금단증상의 예방 및 치료를 위한 산조인 추출물을 함유하는 조성물
EP3009138B1 (fr) * 2014-09-01 2019-05-01 Shyam Prasad Kodimule Extrait de mangifera pour la gestion de l'obésité et/ou du poids

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of WO2018130549A1 *
SHIFFMAN SAUL ET AL: "Nondaily smokers' experience of craving on days they do not smoke.", JOURNAL OF ABNORMAL PSYCHOLOGY, vol. 124, no. 3, 1 August 2015 (2015-08-01), US, pages 648 - 659, XP093204260, ISSN: 0021-843X, DOI: 10.1037/abn0000063 *

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